RKI-1447

RKI-1447

Catalog Number:
L002368846APE
Mfr. No.:
APE-A3771
Price:
$258
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      • Overview
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          Background

          RKI-1447 is a potent inhibitor of ROCK 1 and 2 (Rho-associated protein kinase 1 and 2).
          ROCK is a serine-threonine kinase, which regulates cell shape and movement via acting on cytoskeleton.
          RKI-1447 specifically and dose-dependently inhibits ROCK1 and ROCK2. RKI-1447 inhibited the phosphorylation of the ROCK substrates MLC-2 and MYPT-1 in human cancer cells. However, it does not affect the phosphorylation of the AKT, MEK, and S6 kinase at a high concentrations of 10 μmol/L. It indicated a high specificity. Additionally, it was also observed that RKI-1447 selectively suppressed ROCK-mediated cytoskeleton re-organization following LPA stimulation, but does not affect PAK-meditated lamellipodia and filopodia formation following PDGF and Bradykinin stimulation. RKI-1447 inhibited migration, invasion and anchorage-independent tumor growth of breast cancer cells [1]
          In mouse model, tumors were monitored at the time of tumor onset and the beginning of treatment (once a day for 14 days) with vehicle (20% HPCD) or RKI-1447 (200 mg/kg/day), when tumor volumes reached 75 to 2,300 mm3. Tumors from mice treated with vehicle increased in average tumor volume of 68.3% but tumors from mice treated with the RKI-1447 increased in average tumor volume of only 8.8%. Thus, RKI-1447 inhibited mammary tumor growth by 87% [1].

      • Properties
        • Alternative Name
          RKI 1447;RKI1447; 1-[(3-hydroxyphenyl)methyl]-3-(4-pyridin-4-yl-1,3-thiazol-2-yl)urea
          CAS Number
          1342278-01-6
          Molecular Formula
          C16H14N4O2S
          Molecular Weight
          326.37
          Appearance
          A solid
          Purity
          99.52%
          Solubility
          insoluble in H2O; ≥16.3 mg/mL in DMSO; ≥6.32 mg/mL in EtOH with gentle warming and ultrasonic
          Storage
          Store at -20°C

          * For Research Use Only

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